NR 566 Week 6 Study Guide

 Know the pharmacodynamics, pharmacotherapeutics, clinical use, drug interactions, and ADRs for:
Erectile dysfunction (ED) drugs, Estrogens and Progesterone, and Antiandrogen drugs
 Androgen drugs
o Testosterone is the primary male androgen
o Responsible for:
 Growth, maturation, and maintenance of male sex organs and secondary sexual
characteristics
 Skeletal growth spurt in adolescence and termination of linear growth by fusion of the
epiphyseal growth plate
 Activation of sebaceous glands (acne during puberty)
 Enhances production of erythropoietic stimulating factor, increased RBCs production
 Libido
o Androgen Drugs: testosterone propionate (in oil, DepoTesterone), testosterone enanthate (in oil,
Delatestryl), testosterone cypionate (in oil, Depo-Testosterone), methyltestosterone (Android,
Methitest, Testred, Virilon), testosterone gel (AndroGel 1%, AndroGel 1.62%, Axiron, Testium),
fluoxymesterone, TD testosterone (Testoderm, Androderm), and buccal testosterone (Striant)
 Used to treat Indicated for the symptomatic Tx of
 1) deficiency states in males associated with hypogonadism and
 2) in both sexes for d/os such as CA and HIB, Tx libido, endometriosis, and
postmenopausal symptoms in women, have been used illicitly to enhance athletic
performance and increase muscle mass
o Contraindicated: male breast CA, prostate CA, and Pregnancy (Category X), and lactation
 Antiandrogens: several different categories
o Androgen hormone inhibitors (5-alpha-reductase inhibitors)
 Drugs: Finasteride (Propecia, Proscar) and dutasteride (Avodart)
 MOA: Block conversation of testosterone to dihydrotesterone
 Used to Tx BPH
 PSA levels and digital prostate examination are required monitoring for men on these agents
 Finasteride (Propecia, Proscar):
 Extensive hepatic metabolism
 BPH: 5mg/day, 6 to 12 months of therapy until therapeutic response
o Regression of prostate size increased urinary flow, and improve BPH
symptoms
 Approved for Male pattern baldness: 1 mg/day, three months until results
 Stopping the drugs reverses the effect within 12 months
 ADRs: decreased libido, impotence (can occur at both doses)
 Dutasteride (Avodart)
 Inhibits both type 1 and 2 (5-alpha-reductase)
 Peak clinical effect 6 to 12 months of therapy
 Extensively metabolized in the liver (CYP3A4 and CYP3A5)
 Used to Tx BPH
 Absorbed through the skin, women who are pregnant or may become pregnant should
not handle dutasteride capsules r/t risk of fetal anomaly to a male fetus
 ADR: decreased libido and impotence
o Gonadotropin-releasing hormone analogue: luteinizing hormone-releasing hormone antagonist
 Leuprolide acetate (Lupron)
 Create a reversible chemical orchiectomy state in males and an oophorectomy state in
females
 Used to Tx: advanced prostatic CA and for management of endometriosis and uterine
leiomyomata (fibroids)
 1 mg SC daily or IM every 3 months (depot formulation)
 Increased suppression when used with flutamide (direct antiandrogen)
 Peds: Tx central precocious puberty
 Women: reducing uterine fibroids, endometriosis, and PCOS (pain relief, regain fertility)
o Direct antiandrogens
 Flutamide (Eulexin), bicalutamide (Casodex), and nilutamide (Nilandron)
 Inhibit androgen uptake or nuclear binding of androgen at target tissues
 Uses as part of combo therapy Tx of prostatic carcinoma
 Flutamide: competitive antagonist at the androgen receptor site
 Truly a nonsteroidal agent
 ADRs: gynecomastia and reversible liver toxicity
 Renal doses: less than 29 mL/min
 BLACK BOX WARNING: hepatic failure, hepatic encephalopathy, and death
o Usually within the first 3 months of therapy
o Baseline and monthly LFTs for the first 4 months of therapy and periodically
o D/c if any symptoms of hepatic injury or jaundice develop
o Spironolactone (Aldactone): aldosterone antagonist and inhibitor of 5-alpha-reductase